Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides

Abstract

Here, we investigated the effect of CH₃ to CF₃ substitution on the membrane permeability of peptides. We synthesized a series of peptides with CF₃ groups and corresponding nonfluorinated peptides and measured the membrane permeability of the peptides. As a result, we demonstrated that CH₃ to CF₃ substitution is useful for increasing the membrane permeability of di-/tri-peptides.